127061-41-0

Upstream product

• 6656-49-1 2-methyl-1-nitro-3-(trifluoromethyl)benzene 
• 85-44-9 phthalic anhydride 
• 127061-43-2 (3R-cis)-3-(hydroxy)-1,3,4,5-tetrahydro-4-[4-methoxyphenyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 
• 111604-99-0 [1-(4-Methoxyphenyl)-2-[2-nitro-6-(trifluoromethyl)phenyl]ethyl]propanedioic acid,dimethyl ester 
• 138383-10-5 1,3,4,5-tetrahydro-6-(trifluoromethyl)-3-(methoxycarbonyl)-4-(4-methoxyphenyl)-2H-1-benzazepin-2-one 
• 138337-24-3 (3R,4R)-3-Hydroxy-4-(4-methoxy-phenyl)-2-oxo-6-trifluoromethyl-2,3,4,5-tetrahydro-1H-benzo[b]azepine-3-carboxylic acid methyl ester 
• 133963-42-5 (3R,4S)-3-Hydroxy-4-(4-methoxy-phenyl)-6-trifluoromethyl-1,3,4,5-tetrahydro-benzo[b]azepin-2-one 
• 111605-05-1 [2-(2-amino-6-trifluoromethylphenyl)-1-(4-methoxyphenyl)ethyl]propanedioic acid,dimethyl ester 
• 7443-25-6 dimethyl 2-(4-methoxybenzylidene)malonate 

Downstream Products

• 127061-43-2 (3R-cis)-3-(hydroxy)-1,3,4,5-tetrahydro-4-[4-methoxyphenyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 
• 128510-26-9 <3R-<1(S^*),3α,4α>>-3-(acetyloxy)-1-<<(benzyloxycarbonyl)-2-pyrrolidinyl>methyl>-1,3,4,5-tetrahydro-4-(4-methoxyphenyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 
• 133963-43-6 [3R-(1(S^*),3α,4α)]-3-(acetyloxy)-1,3,4,5-tetrahydro-4-(4-methoxyphenyl)-1-(2-pyrrolidinylmethyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 
• 134932-93-7 <3R-<1(S^*),3α,4α>>-1-<<(benzyloxycarbonyl)-2-pyrrolidinyl>methyl>-1,3,4,5-tetrahydro-3-hydroxy-4-(4-methoxyphenyl)-6-(trifluoromethyl)-2H-1-benzazepin-2-one 

Relevant academic research and scientific papers

Chemoenzymatic synthesis of benzazepinone calcium channel blocking agents

The synthesis of a 6-trifluoromethyl-benzazepin-2-one derivative (3) from readily available nitro-toluene (4) is described.This synthetic route requires an enantio- and stereo-selective microbial reduction of racemic 13 to form (3R,4S)-cis-alcohol (10).Compound 3 is potent calcium channel blocking agent both in vitro and in vivo.

Resolution process for benzazepine intermediates

In accordance with the present invention an improved process for preparing resolved compounds of the formula STR1 wherein R1 is hydrogen or acetyl.